Pharmacology

Question 1

pirfenidone

Answer 1

inhibits TGF-beta mediated collagen synthesis

tx for IPF

decreased rate of FVC decline, may decrease mortality

side fx: nausea, photosensitivity, rash, dyspepsia, elevated LFTs

Question 2

nintedanib

Answer 2

multiple tyrosine kinase inhibitor

tx for IPF

decreased rate of FVC decline, may decrease exacerbations

side fx: nausea, vomiting, elevated LFTs

Question 3

steps of asthma management, GINA guidelines?

Answer 3

1. watch pt use inhaler, discuss adherence/barriers
2. confirm dx asthma
3. remove RF if possible, assess/manage comorbidities
4. tx step up
5. refer to specialist`

Question 4

what are the two classes of beta agonists?

Answer 4

short acting (rescue inhlaer) and long acting (daily controller)

Question 5

mechanism of beta agonists?

Answer 5

GPCRs activate adenylyl cyclase –> convert ATP to cAMP –> cause bronchodilation

increase vasodilation, bronchodilation, liver glycogenolysis.

side fx tachycardia, anxiety

Question 6

do we need to worry about beta receptor cross over effects?

Answer 6

nope!

Question 7

LABA and LAMA are first line therapy for what disease?

Answer 7

COPD

can use only one or both

Question 8

are LABA and LAMA first line therapy for asthma

Answer 8

NO. only after ICS

Question 9

why is LABA/LAMA NOT first line therapy for asthma?

Answer 9

risk of exacerbations.

note: together there is better control of asthma. great as add on therapy in addition to ICS

Question 10

what is the mechanism of action of muscarinic receptor antagonists?

Answer 10

ACh binds muscarinic and nicotinic receptors.

reversibly inhibit effects of ACh on M3 muscarinic receptor –> causes bronchodilation

Question 11

what are side effects of anti cholinergic drugs?

Answer 11

unilateral dilated pupil bc getting out from mask

imp: should see if on other anticholinergic meds bc increase risk of side effects

flushing, confusion, hyperthermia, dry mouth, urinary retention, tachycardia

Question 12

is there a role for anticholinergics in asthma management?

Answer 12

as alternative salvage therapy

Question 13

what is the mechanism of inhaled corticosteroids?

Answer 13

bind glucocorticoid receptor in cytoplasm and enter nucleus to act as TF for antiinflammatory effects.

decrease inflammatory signals and cells. decrease mucus secretion and leakage from endothelium. increase beta2 receptors on airway smooth muscle

Question 14

what is frontline tx for asthma?

Answer 14

low dose ICS

Question 15

what is an important adverse effect of ICS?

Answer 15

thrush

also increased risk of pneumonia, hoarse voice, skin bruising

Question 16

can ICS be used in COPD?

Answer 16

yes if ongoing sxs despite LABA/LAMA

Question 17

what is the mechanism of leukotriene antagonists?

Answer 17

zileuton: selective and specific 5-lipoxygenase inhibitor. prevents conversion of arachidonic acid to leukotriene A4

montelukast and zafirlukast: selective, reversible antagonists of cysteinyl leukotriene-1-receptor, blocks final step in leukotriene pathway

prevent leukotriene pathway which promotes smooth muscle constriction, eosinophil migration, and edema

Question 18

why do doctors like montelukast?

Answer 18

broad indications (children >1 year old)
minimal drug drug interactions
favorable side effect profile

Question 19

what patients would receive leukotriene receptor antagonists?

Answer 19

asthma pts as add on therapy

Question 20

what is the mech of action for phosphodiesterase-4 inhibitors (rofumilast)?

Answer 20

prevent breakdown of cAMP

this decreases inflamm cell activity, inhibits fibrosis, and relaxes smooth muscle

Question 21

who gets phosphodiesterase-4 inhibitors (rofumilast)?

Answer 21

late stage COPD pts. if LAMA/LABA/ICS still have frequent exacerbations

not used in asthma

Question 22

side effects of rofumilast (PDE-4 inhib)

Answer 22

GI related

Question 23

indications for theophylline?

Answer 23

asthma pts as add on therapy
narrow therapeutic window and can cause fatal arrythmias and seizures at toxic levels

(also called methylxanthine- nonselective PDE inhibitor)

Question 24

Bupropion (aka wellbutrin)

Answer 24

blocks neural reuptake of dopamine and/or norepi

contraindicated in pts with seizure hx

start at least 7 days before quit date

Question 25

varenicline

Answer 25

partial agonist/antagonist of alpha-4-beta-2 subunit of nicotinic acetylcholine receptor

side effects: nausea, insomnia/vivid dreams

dose adjustment in renal failure

FDA removed black box warning for neuropsychiatric side effects

start at least 7 days before quit